Therapeutic Targets Database
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TTD Target ID: TTDC00193

Target Information
NameNeuropeptide Y receptor type 1    
Type of targetClinical trial target    
SynonymsNPY1-R    
Neuropeptide Y Y(1) receptor    
Neuropeptide Y receptor Y1    
Neuropeptide Y-Y1 receptor    
DiseaseAnalgesics
[ICD9: 338   ICD10: R52]
[1]
Anxiety disorder, unspecified
[ICD9: 300   ICD10: F40-F42]
[1]
Cardiovascular disease, unspecified
[ICD9: 390-459   ICD10: I00-I99]
[1]
Convulsions
[ICD9: 780.3   ICD10: R56.0]
[1]
Drug dependence
[ICD9: 303-304   ICD10: F10.2-F19.2]
[1]
Metabolic disorder, unspecified
[ICD9: 270-279   ICD10: E70-E89]
[1]
Obesity
[ICD9: 278   ICD10: E66]
[2]
Pain, unspecified
[ICD9: 338,780   ICD10: R52, G89]
[1]
Rhinitis
[ICD9: 472.0, 477   ICD10: J00, J30, J31.0]
[1]
Drug(s)Benzylamine derivativePhase IEating disorder (bulimia) Obesity Hypertension Congestive heart failure[3]
GI-264879APreclinicalObesity[4]
PD-160170PreclinicalHypertension. Obesity, Heart disease[4]
BioChemical ClassG-protein coupled receptor (rhodopsin family)    
PathwayNeuroactive ligand-receptor interaction
UniProt IDP25929
PDB Structure2F1U; 2IIL.    
FunctionReceptor for neuropeptide y and peptide yy. The rank order of affinity of this receptor for pancreatic polypeptides is npy > [pro-34] pyy, pyy and [leu-31, pro-34] npy > npy (2-36) > [ile-31, gln-34] pp and pyy (3-36) > pp > npy free acid.    
SequenceMNSTLFSQVENHSVHSNFSEKNAQLLAFENDDCHLPLAMIFTLALAYGAVIILGVSGNLA LIIIILKQKEMRNVTNILIVNLSFSDLLVAIMCLPFTFVYTLMDHWVFGEAMCKLNPFVQ CVSITVSIFSLVLIAVERHQLIINPRGWRPNNRHAYVGIAVIWVLAVASSLPFLIYQVMT DEPFQNVTLDAYKDKYVCFDQFPSDSHRLSYTTLLLVLQYFGPLCFIFICYFKIYIRLKR RNNMMDKMRDNKYRSSETKRINIMLLSIVVAFAVCWLPLTIFNTVFDWNHQIIATCNHNL LFLLCHLTAMISTCVNPIFYGFLNKNFQRDLQFFFNFCDFRSRDDDYETIAMSTMHTDVS KTSLKQASPVAFKKINNNDDNEKI
Target ValidationClick to Find Target Validation Information.    
Inhibitor4- (4-butylpiperidin-1-yl)-1-o-tolylbutan-1-one[5]
AcPYY (22-36)[6]
Adp[-Trp-Arg-Nva-Arg-Tyr-NH2]2[7]
BIBP-3226[8]
BMS-189323[9]
BMS-245782[9]
ECONAZOLE NITRATE[10]
H-[Trp-Arg-Nva-Arg-Tyr]2-NH2[7]
H-[Trp-Arg-Nva-Arg-Tyr]3-NH2[7]
LRHYLNLLTRQRY-NH2[11]
N-arylpiperazine derivative[9]
N-arylpiperazine derivative[9]
N-arylpiperazine derivative[9]
N-arylpiperazine derivative[9]
N-arylpiperazine derivative[9]
N-arylpiperazine derivative[9]
N-arylpiperazine derivative[9]
N-arylpiperazine derivative[9]
N-arylpiperazine derivative[9]
N-arylpiperazine derivative[9]
NEUROPEPTIDE-Y[12]
PYY (22-36)[6]
PYY (3-36)[6]
Pim[-Trp-Arg-Nva-Arg-Tyr-NH2]2[7]
Sub[-Trp-Arg-Nva-Arg-Tyr-NH2]2[7]
Sub[-Tyr-Arg-Leu-Arg-Tyr-NH2]2[7]
[Cys-Trp-Arg-Nva-Arg-Tyr-NH2]2[7]
neuropeptide Y[13]
AntagonistBIBO3304[14]
BIBP 3226[15][16]
BMS-193885[17]
Benzylamine derivative[3]
GI-264879A[4]
J-104870[18]
NPY-1 antagonist[3]
PD-160170[4]
S-19528[3]
S-25585[3]
SR 120819A[19]
Cross References 3D Structure
Related Literature
On-Line Medical Dictionary
Ref 1Neuropeptide Y and its receptors as potential therapeutic drug targets. Clin Chim Acta. 2002 Dec;326(1-2):3-25. To Reference
Ref 2Neuropeptide Y receptors as targets for anti-obesity drug development: perspective and current status. Eur J Pharmacol. 2002 Apr 12;440(2-3):173-87. To Reference
Ref 3Emerging drugs for eating disorder treatment. Expert Opin Emerg Drugs. 2006 May;11(2):315-36. To Reference
Ref 4Emerging drugs for obesity: linking novel biological mechanisms to pharmaceutical pipelines. Expert Opin Emerg Drugs. 2005 Aug;10(3):643-60. To Reference
Ref 5J Med Chem. 2010 Sep 9;53(17):6386-97.Discovery of N-{1-[3-(3-oxo-2,3-dihydrobenzo[1,4]oxazin-4-yl)propyl]piperidin-4-yl}-2-phenylacetamide (Lu AE51090): an allosteric muscarinic M1 receptor agonist with unprecedented selectivity and procognitive potential. To Reference
Ref 6Bioorg Med Chem Lett. 2007 Jan 15;17(2):538-41. Epub 2006 Oct 7.Identification of selective neuropeptide Y2 peptide agonists. To Reference
Ref 7J Med Chem. 2006 Apr 20;49(8):2661-5.Neuropeptide Y (NPY) Y4 receptor selective agonists based on NPY(32-36): development of an anorectic Y4 receptor selective agonist with picomolar affinity. To Reference
Ref 8Bioorg Med Chem. 2010 Sep 1;18(17):6292-304. Epub 2010 Jul 16.N(G)-Acyl-argininamides as NPY Y(1) receptor antagonists: Influence of structurally diverse acyl substituents on stability and affinity. To Reference
Ref 9Bioorg Med Chem Lett. 2004 Dec 20;14(24):5975-8.Isosteric N-arylpiperazine replacements in a series of dihydropyridine NPY1 receptor antagonists. To Reference
Ref 10Bioorg Med Chem Lett. 2010 Dec 15;20(24):7331-6. Epub 2010 Oct 21.In silico identification and biochemical evaluation of novel inhibitors of NRH:quinone oxidoreductase 2 (NQO2). To Reference
Ref 11Bioorg Med Chem Lett. 2007 Apr 1;17(7):1916-9. Epub 2007 Jan 24.A long-acting selective neuropeptide Y2 receptor PEGylated peptide agonist reduces food intake in mice. To Reference
Ref 12J Med Chem. 2008 Dec 25;51(24):8168-72.Guanidine-acylguanidine bioisosteric approach in the design of radioligands: synthesis of a tritium-labeled N(G)-propionylargininamide ([3H]-UR-MK114) as a highly potent and selective neuropeptide Y Y1 receptor antagonist. To Reference
Ref 13J Nat Prod. 2009 Dec;72(12):2172-6.5-OHKF and NorKA, depsipeptides from a Hawaiian collection of Bryopsis pennata: binding properties for NorKA to the human neuropeptide Y Y1 receptor. To Reference
Ref 14Neuropeptide Y induced modulation of dopamine synthesis in the striatum. Regul Pept. 2005 Jul 15;129(1-3):73-8. To Reference
Ref 15Effects of a selective neuropeptide Y Y(1) receptor antagonist BIBP 3226 on double peaked vasoconstrictor responses to periarterial nerve stimulation in canine splenic arteries. Br J Pharmacol. 2000 Aug;130(7):1699-705. To Reference
Ref 16Intracerebroventricular injection of a neuropeptide Y-Y1 receptor agonist increases while BIBP3226, a Y1 antagonist, reduces the infarct volume following transient middle cerebral artery occlusion in rats. Neuroscience. 2003;116(1):119-26. To Reference
Ref 17Dihydropyridine neuropeptide Y Y(1) receptor antagonists. Bioorg Med Chem Lett. 2002 Feb 11;12(3):379-82. To Reference
Ref 18The novel neuropeptide Y Y(1) receptor antagonist J-104870: a potent feeding suppressant with oral bioavailability. Biochem Biophys Res Commun. 1999 Dec 9;266(1):88-91. To Reference
Ref 19SR 120819A, an orally-active and selective neuropeptide Y Y1 receptor antagonist. FEBS Lett. 1995 Apr 3;362(2):192-6. To Reference



 

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